An article Structure-Based Design of a Bromodomain and Extraterminal Domain (BET) Inhibitor Selective for the N-Terminal Bromodomains That Retains an Anti-inflammatory and Antiproliferative Phenotype WOS:000571493400008 published article about SMALL-MOLECULE; DISCOVERY; POTENT; PROTEIN; FAMILY; BRD4; IDENTIFICATION; OPTIMIZATION; CHROMATIN; RVX-208 in [Wellaway, Christopher R.; Bamborough, Paul; Bernard, Sharon G.; Chung, Chun-wa; Craggs, Peter D.; Cutler, Leanne; Demont, Emmanuel H.; Evans, John P.; Gordon, Laurie; Karamshi, Bhumika; Lewis, Antonia J.; Lindon, Matthew J.; Mitchell, Darren J.; Rioja, Inmaculada; Soden, Peter E.; Taylor, Simon; Watson, Robert J.; Willis, Rob; Woolven, James M.; Wyspianska, Beata S.; Kerr, William J.; Prinjha, Rab K.] GSK, Med Res Ctr, Stevenage SG1 2NY, Herts, England in 2020.0, Cited 46.0. HPLC of Formula: C7H8O. The Name is Benzyl Alcohol. Through research, I have a further understanding and discovery of 100-51-6
The bromodomain and extraterminal domain (BET) family of epigenetic regulators comprises four proteins (BRD2, BRD3, BRD4, BRDT), each containing tandem bromodomains. To date, small molecule inhibitors of these proteins typically bind all eight bromodomains of the family with similar affinity, resulting in a diverse range of biological effects. To enable further understanding of the broad phenotype characteristic of pan-BET inhibition, the development of inhibitors selective for individual, or sets of, bromodomains within the family is required. In this regard, we report the discovery of a potent probe molecule possessing up to 150-fold selectivity for the N-terminal bromodomains (BD1s) over the C-terminal bromodomains (BD2s) of the BETs. Guided by structural information, a specific amino acid difference between BD1 and BD2 domains was targeted for selective interaction with chemical functionality appended to the previously developed I-BET151 scaffold. Data presented herein demonstrate that selective inhibition of BD1 domains is sufficient to drive anti-inflammatory and antiproliferative effects.
Welcome to talk about 100-51-6, If you have any questions, you can contact Wellaway, CR; Bamborough, P; Bernard, SG; Chung, CW; Craggs, PD; Cutler, L; Demont, EH; Evans, JP; Gordon, L; Karamshi, B; Lewis, AJ; Lindon, MJ; Mitchell, DJ; Rioja, I; Soden, PE; Taylor, S; Watson, RJ; Willis, R; Woolven, JM; Wyspianska, BS; Kerr, WJ; Prinjha, RK or send Email.. HPLC of Formula: C7H8O
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Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles